Rentosertib
Based on 1 Customer Validation
Rentosertib (INS018 055) (compound 112) is the orally active TNIK and MAP4K4 inhibitor with IC50 values of 12-120, 12-120 nM, respectively.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.96%
- CAS No.: 2828567-39-9
- Formule: C27H30FN7O
- Masse moléculaire:487.57
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
MAP4K4 12-120 nM (IC50) |
TNIK 12-120 nM (IC50) |
In Vitro
Rentosertib (INS018 055) (0-3 μM, 72 h) reduces TGF-β-induced α-SMA protein expressio with an IC50 of 27.14 nM in MRC-5 cell[2].
Rentosertib (INS018 055) (0-3 μM, 72 h) decreases the expression of N-cadherin, p-SMAD2/SMAD3, increases the expression of E-cadherin, and inhibits TGF-β-induced epithelial-to-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transition (FMT) in A549 cell[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:A549
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Concentration:0-3 μM
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Incubation Time:72 h
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Result:Decreased the expression of N-cadherin and p-SMAD2/SMAD3, and increased the expression of E-cadherin.
In Vivo
Rentosertib (INS018 055) (3-30 mg/kg, po, single dose) reduces the number of lymphocytes in bronchoalveolar lavage fluid (BALF), inhibits the expressions of pro-inflammatory cytokines, and exhibits anti-inflammatory effect in LPS (HY-D1056)-induced mouse acute lung injury model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Bleomycin (HY-17565)-induced mouse pulmonary fibrosis models[2]
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Dosage:3-30 mg/kg
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Administration:po, twice a day for 2 weeks
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Result:Improved lung function, reduced the area of pulmonary fibrosis, and reduced the expression of α-SMA and collagen I.
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Animal Model:LPS (HY-D1056)-induced mouse acute lung injury model[2]
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Dosage:3-30 mg/kg
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Administration:po, single dose
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Result:Reduced the number of lymphocytes in bronchoalveolar lavage fluid (BALF), reduced the levels of IL-1β, IL-6, IL-7 and TNF-α, and increased the level of IL-4.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2828567-39-9
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Appearance Solid
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Masse moléculaire 487.57
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Formule C27H30FN7O
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Color White to light yellow
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SMILES
O=C(C1=CN=C(C2=C(C3=CC=C(C=C3)F)N=CN2C(C)C)N1)NC4=CC=C(N5CCN(CC5)C)C=C4
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Synonyms
INS018_055; TNIK&MAP4K4-IN-2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (205.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.0510 mL | 10.2549 mL | 20.5099 mL | 51.2747 mL |
| 5 mM | 0.4102 mL | 2.0510 mL | 4.1020 mL | 10.2549 mL | |
| 10 mM | 0.2051 mL | 1.0255 mL | 2.0510 mL | 5.1275 mL | |
| 15 mM | 0.1367 mL | 0.6837 mL | 1.3673 mL | 3.4183 mL | |
| 20 mM | 0.1025 mL | 0.5127 mL | 1.0255 mL | 2.5637 mL | |
| 25 mM | 0.0820 mL | 0.4102 mL | 0.8204 mL | 2.0510 mL | |
| 30 mM | 0.0684 mL | 0.3418 mL | 0.6837 mL | 1.7092 mL | |
| 40 mM | 0.0513 mL | 0.2564 mL | 0.5127 mL | 1.2819 mL | |
| 50 mM | 0.0410 mL | 0.2051 mL | 0.4102 mL | 1.0255 mL | |
| 60 mM | 0.0342 mL | 0.1709 mL | 0.3418 mL | 0.8546 mL | |
| 80 mM | 0.0256 mL | 0.1282 mL | 0.2564 mL | 0.6409 mL | |
| 100 mM | 0.0205 mL | 0.1025 mL | 0.2051 mL | 0.5127 mL |
Rentosertib Related Classifications
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